137473-27-9Relevant articles and documents
Oxidative alkoxycarbonylation of terminal alkenes with carbazates
Su, Yu-Han,Wu, Zhao,Tian, Shi-Kai
supporting information, p. 6528 - 6530 (2013/07/26)
A range of terminal alkenes smoothly underwent palladium-catalyzed oxidative alkoxycarbonylation with carbazates under an oxygen atmosphere to afford structurally diverse α,β-unsaturated esters in moderate to good yields with excellent regioselectivity and E selectivity.
An efficient enantioselective synthesis of florfenicol based on sharpless asymmetric dihydroxylation
Wang, Zhong-Hua,Zheng, Chen,Li, Feng,Zhao, Lei,Chen, Fen-Er,He, Qiu-Qin
, p. 699 - 704 (2012/04/04)
An efficient and highly enantioselective synthesis of florfenicol- via a new intermediate threo-dihydroxy ester, with a Sharpless asymmetric dihydroxylation as the key step, is reported. A ring-opening/reduction strategy avoids the formation of a chlorinated byproduct that occurs in Schumachers phenyloxazoline procedure. The overall yield of florfenicol by this new process is 23% based on 4-(methylsulfonyl)benzaldehyde. Georg Thieme Verlag Stuttgart · New York.
Synthesis and antifungal activities of R-102557 and related dioxane- triazole derivatives
Oida, Sadao,Tajima, Yawara,Konosu, Toshiyuki,Nakamura, Yoshie,Somada, Atsushi,Tanaka, Teruo,Habuki, Shinobu,Harasaki, Tamako,Kamai, Yasuki,Fukuoka, Takashi,Ohya, Satoshi,Yasuda, Hiroshi
, p. 694 - 707 (2007/10/03)
Novel triazole compounds with a dioxane ring were synthesized. Condensation of the diol precursor 10 with various aromatic aldehydes 11 - 13 under acidic conditions afforded a series of dioxane-triazole compounds 14 - 16. The antifungal activities of the compounds 14 - 16 were evaluated in vivo in mice infection models against Candida and Aspergillus species. High activities were seen for the derivatives with one or two double bond(s) and an aromatic ring substituted with an electron-withdrawing group in the side chain. Among the derivatives, R-102557 (16R: Ar=4-(2,2,3,3- tetrafluoropropoxy)phenyl) showed excellent in vivo activities against Candida, Aspergillus and Cryptococcus species. It also showed high tolerance in a preliminary toxicity study in rats.